Issue 6, 2011
From the journal:

MedChemComm

N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators†

Zhiqing Liu,‡a   Qingzhang Zhu,‡b   Fuying Li,§a   Lina Zhang,b   Ying Leng*b  and  Ao Zhang*a  

* Corresponding authors

a Synthetic Organic & Medicinal Chemistry Laboratory (SOMCL), Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai, China
E-mail: aozhang@mail.shcnc.ac.cn
Fax: +86-21-50806035
Tel: +86-21-50806035

b State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai, China
E-mail: yleng@mail.shcnc.ac.cn
Fax: +86-21-50806059
Tel: +86-21-50806059

Abstract

A series of novel arylacetamides were designed to further explore the GK binding property at the aminothiazole C5 position. The C5-amide substituted aminothiazoles 7a–f generally displayed decreased potency, whereas most of the C5-triazole substituted aminothiazoles retained good GK potency. Triazole 15 with a hydroxyethyl side chain was the most potent among the current series possessing an EC50 value of 0.18 μM. Its R-enantiomerR-15 showed similar potency (0.22 μM) that deserves for further evaluation.

Graphical abstract: N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators

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Article information

DOI
https://doi.org/10.1039/C1MD00002K
Article type
Concise Article
Submitted
05 Jan 2011
Accepted
22 Mar 2011
First published
14 Apr 2011

Med. Chem. Commun., 2011,2, 531-535

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N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators

Z. Liu, Q. Zhu, F. Li, L. Zhang, Y. Leng and A. Zhang, Med. Chem. Commun., 2011, 2, 531 DOI: 10.1039/C1MD00002K

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